- Preparation method and application of peramivir related substances
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The invention discloses a preparation method and application of a peramivir related substance I. The related substance can be used as a peramivir impurity reference substance for separating and determining peramivir and the peramivir related substance I by a high performance liquid chromatography method. The preparation method provided by the invention has the advantages of mild reaction conditions and simple post-treatment, and can be used for large-scale preparation of the compound shown as the formula I with purity meeting the requirements to serve as an impurity reference substance for peramivir quality research.
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- Synthesis method of 3+2 closed ring
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The invention discloses a synthesis method of a 3+2 closed ring. According to the method, chiral induction is enhanced under the spatial steric effect of bridge ring molecules, so that a ring closingreaction has efficient spatial selectivity. The method is applied to synthesis of peramivir and has the characteristics that the synthesis route is short, the stereoselectivity is high and the operation procedure is convenient.
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- Facile synthesis of the neuraminidase inhibitor peramivir
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An improved and convenient synthetic route for the synthesis of peramivir has been developed with a total 34% yield. The process was improved from previous methods in three key reaction steps including 1,3-dipolar cycloaddition, reductive ring cleavage of
- Jia, Fei,Hong, Juan,Sun, Ping-Hua,Chen, Jian-Xin,Chen, Wei-Min
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p. 2641 - 2647
(2013/07/26)
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- A NOVEL PROCESS FOR THE PREPARATION OF PERAMIVIR AND INTERMEDIATES THEREOF
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The present invention relates to a novel process for preparing peramivir formula (I) or a pharmaceutically acceptable salt thereof, and to intermediates used therein.
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- (1S, 2S, 3S, 4R)-3-Y(1S)-1-ACETYLAMINO-2-ETHYL-BUTYL¨-4-GUANIDINO-2- HYDROXYL-CYCLOPENTYL-1-CARBOXYLIC ACID HYDRATES AND PHARMACEUTICAL USES THEREOF
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The present invention relates to (1S,2S,3S,4R)-3-[(1S)-1-acetylamino-2-ethyl-butyl]-4-guanidino-2-hydroxy-cyclopentyl-1-carboxylic acid hydrates compounds, preparing methods thereof, pharmaceutical compositions containing said compounds and preparing methods thereof, and the clinical uses of said compounds as neuramidinase inhibitors for anti-influenza.
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Page/Page column 6; 12-13
(2010/06/15)
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- Stereoselective total synthesis of racemic BCX-1812 (RWJ-270201) for the development of neuraminidase inhibitors as anti-influenza agents
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A convergent and versatile racemic total synthesis of the anti-influenza agent BCX-1812 (RWJ-270201) was accomplished on the basis of a sequence of stereoselective reactions. Despite intensive research to develop neuraminidase inhibitors to treat infections due to influenza, currently available agents are still in the need of optimization with respect to selectivity and potency, as well as to minimize adverse effects. Our synthetic approach, introduced in this report, is highly exploitable for further derivatization due to flexibility that will eventually accommodate diversified substituents. In addition, the size of the core ring can be varied depending on the size of the diene used for the preparation of the key cycloadduct 10 using an acylnitroso-based hetero-Diels-Alder reaction. Elaboration of 10 to methyl ester 14 followed by a precedented [3+2] dipolar cycloaddition gave bicyclic isoxazoline 17 in a regio- and stereoselective fashion. Incorporation of the peripheral guanidino group and subsequent deprotection provided the target molecule. The details of the synthesis are described herein.
- Mineno, Tomoko,Miller, Marvin J.
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p. 6591 - 6596
(2007/10/03)
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